Docetaxel (1) is obtained by the structure modification based on the paclitaxel. The docetaxel promises a broad range of anti-leukemic and tumor-inhibiting activity, and has been considered one of the most effective anticancer drugs till now, with the anticancer activity 1.3- to 12-fold more potent than paclitaxel. Docetaxel has the same complex structure as paclitaxel, including various function groups and chiral centers, which lead to great difficulty of the total synthesis. Semi-synthesis is the most effective chemical method for preparing docetaxel.

The semi-synthesis method reported in the references and patents may be divided into two categories. The first is that following the condensation reactions of protected 10-deacetylbaccatin III and five-membered oxazolidine side chain, the compound is de-protected through hydrolyzing to yield docetaxel. (U.S. Pat. No. 6,900,342); the second is that following the coupling reactions of protected 10-deacetylbaccatin III with β-lactam under extremely low temperature in the presence of strong base (such as n-butyllithium), the compound is de-protected through hydrolyzing to yield docetaxel. (See the following scheme in FIGS. 1-2.)
In the first method (see FIG. 1), the condensation condition is milder, but a great amount of condensation reagent DCC(N,N′-dicyclohexyl carbodiimide) will be used and cause many difficulties in the following purification.
In the second method (see FIG. 2), the condition is more rigorous, because of the using of strong base, mishandling will cause decomposition of the protected 10-deacetylbaccatin III and waste of the expensive raw material. Moreover, the excessive side chain needed in this method not only increases the difficulty of the following purification, but also increases the cost of manufacture.